Synthesis and evaluation of novel analogues of mangiferin as potent antipyretic

<正>Objective:To screen different analogues of mangiferin pharmacologically for antipyretic activity. Methods:The naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the elhanolic extract of stem bark of Mangifera indica.Mangiferin was further co...

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Veröffentlicht in:Asian Pacific journal of tropical medicine 2011-11, Vol.4 (11), p.866-869
Hauptverfasser: Kant Singh, Shashi, Sinha, Saurabh K, Prasad, SK, Kumar, R, Bithu, Bhawani S, Sadish Kumar, S, Singh, P
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container_end_page 869
container_issue 11
container_start_page 866
container_title Asian Pacific journal of tropical medicine
container_volume 4
creator Kant Singh, Shashi
Sinha, Saurabh K
Prasad, SK
Kumar, R
Bithu, Bhawani S
Sadish Kumar, S
Singh, P
description <正>Objective:To screen different analogues of mangiferin pharmacologically for antipyretic activity. Methods:The naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the elhanolic extract of stem bark of Mangifera indica.Mangiferin was further converted to 5-(N-phenylamino methyleno) mangiferin.5-(N-p-chlorophenylamino methyleno) mangiferin,5-(N-2-methyl phenylamino methyleno) mangiferin.5-(N-p-methoxy phenylamino methyleno) mangiferin.5-(N,N-diphenylamino methyleno) mangiferin,5-(N-α-napthylamino methyleno) mangiferin and 5-(N-4-methyl phenylamino methyleno) mangiferin analogues.The synthesized compounds were further screened for antipyretic activity along with mangiferin at a dose level of 100 and 200 tng/kg.Mangiferin and its analogues were characterized by melting point and R_f value determination and through spectral technique like UV,IR,and NMR spectral analysis.Results:The antipyretic activity of mangiferin as well as all analogues was found to be more significant in at higher dose ie.200 mg/kg which was depicted thmugh a decrease in rectal temperature up to 3 h.Conclusions:The antipyretic activity of mangiferin and its analogues may be attributed to inhibition in synthesis of TNF-αand anti-oxidant activity associated with amelioration of inflammatory actions of cytokines.
doi_str_mv 10.1016/S1995-7645(11)60210-1
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Methods:The naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the elhanolic extract of stem bark of Mangifera indica.Mangiferin was further converted to 5-(N-phenylamino methyleno) mangiferin.5-(N-p-chlorophenylamino methyleno) mangiferin,5-(N-2-methyl phenylamino methyleno) mangiferin.5-(N-p-methoxy phenylamino methyleno) mangiferin.5-(N,N-diphenylamino methyleno) mangiferin,5-(N-α-napthylamino methyleno) mangiferin and 5-(N-4-methyl phenylamino methyleno) mangiferin analogues.The synthesized compounds were further screened for antipyretic activity along with mangiferin at a dose level of 100 and 200 tng/kg.Mangiferin and its analogues were characterized by melting point and R_f value determination and through spectral technique like UV,IR,and NMR spectral analysis.Results:The antipyretic activity of mangiferin as well as all analogues was found to be more significant in at higher dose ie.200 mg/kg which was depicted thmugh a decrease in rectal temperature up to 3 h.Conclusions:The antipyretic activity of mangiferin and its analogues may be attributed to inhibition in synthesis of TNF-αand anti-oxidant activity associated with amelioration of inflammatory actions of cytokines.</description><identifier>ISSN: 1995-7645</identifier><identifier>EISSN: 2352-4146</identifier><identifier>DOI: 10.1016/S1995-7645(11)60210-1</identifier><identifier>PMID: 22078948</identifier><language>eng</language><publisher>India: Elsevier B.V</publisher><subject>Animals ; Antipyretic ; Bark ; Disease Models, Animal ; Dose-Response Relationship, Drug ; Fever - chemically induced ; Fever - drug therapy ; Glycosides - pharmacology ; Glycosides - therapeutic use ; indica ; Mangifera ; Mangifera - chemistry ; Mangifera indica ; Mangiferin ; Mice ; Phytotherapy ; Plant Bark - chemistry ; Plant Extracts - pharmacology ; Plant Extracts - therapeutic use ; Saccharomyces cerevisiae ; Treatment Outcome ; Xanthones - administration &amp; dosage ; Xanthones - chemical synthesis ; Xanthones - pharmacology ; Xanthones - therapeutic use</subject><ispartof>Asian Pacific journal of tropical medicine, 2011-11, Vol.4 (11), p.866-869</ispartof><rights>2011 Hainan Medical College</rights><rights>Copyright © 2011 Hainan Medical College. 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Methods:The naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the elhanolic extract of stem bark of Mangifera indica.Mangiferin was further converted to 5-(N-phenylamino methyleno) mangiferin.5-(N-p-chlorophenylamino methyleno) mangiferin,5-(N-2-methyl phenylamino methyleno) mangiferin.5-(N-p-methoxy phenylamino methyleno) mangiferin.5-(N,N-diphenylamino methyleno) mangiferin,5-(N-α-napthylamino methyleno) mangiferin and 5-(N-4-methyl phenylamino methyleno) mangiferin analogues.The synthesized compounds were further screened for antipyretic activity along with mangiferin at a dose level of 100 and 200 tng/kg.Mangiferin and its analogues were characterized by melting point and R_f value determination and through spectral technique like UV,IR,and NMR spectral analysis.Results:The antipyretic activity of mangiferin as well as all analogues was found to be more significant in at higher dose ie.200 mg/kg which was depicted thmugh a decrease in rectal temperature up to 3 h.Conclusions:The antipyretic activity of mangiferin and its analogues may be attributed to inhibition in synthesis of TNF-αand anti-oxidant activity associated with amelioration of inflammatory actions of cytokines.</description><subject>Animals</subject><subject>Antipyretic</subject><subject>Bark</subject><subject>Disease Models, Animal</subject><subject>Dose-Response Relationship, Drug</subject><subject>Fever - chemically induced</subject><subject>Fever - drug therapy</subject><subject>Glycosides - pharmacology</subject><subject>Glycosides - therapeutic use</subject><subject>indica</subject><subject>Mangifera</subject><subject>Mangifera - chemistry</subject><subject>Mangifera indica</subject><subject>Mangiferin</subject><subject>Mice</subject><subject>Phytotherapy</subject><subject>Plant Bark - chemistry</subject><subject>Plant Extracts - pharmacology</subject><subject>Plant Extracts - therapeutic use</subject><subject>Saccharomyces cerevisiae</subject><subject>Treatment Outcome</subject><subject>Xanthones - administration &amp; 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Methods:The naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the elhanolic extract of stem bark of Mangifera indica.Mangiferin was further converted to 5-(N-phenylamino methyleno) mangiferin.5-(N-p-chlorophenylamino methyleno) mangiferin,5-(N-2-methyl phenylamino methyleno) mangiferin.5-(N-p-methoxy phenylamino methyleno) mangiferin.5-(N,N-diphenylamino methyleno) mangiferin,5-(N-α-napthylamino methyleno) mangiferin and 5-(N-4-methyl phenylamino methyleno) mangiferin analogues.The synthesized compounds were further screened for antipyretic activity along with mangiferin at a dose level of 100 and 200 tng/kg.Mangiferin and its analogues were characterized by melting point and R_f value determination and through spectral technique like UV,IR,and NMR spectral analysis.Results:The antipyretic activity of mangiferin as well as all analogues was found to be more significant in at higher dose ie.200 mg/kg which was depicted thmugh a decrease in rectal temperature up to 3 h.Conclusions:The antipyretic activity of mangiferin and its analogues may be attributed to inhibition in synthesis of TNF-αand anti-oxidant activity associated with amelioration of inflammatory actions of cytokines.</abstract><cop>India</cop><pub>Elsevier B.V</pub><pmid>22078948</pmid><doi>10.1016/S1995-7645(11)60210-1</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record>
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identifier ISSN: 1995-7645
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subjects Animals
Antipyretic
Bark
Disease Models, Animal
Dose-Response Relationship, Drug
Fever - chemically induced
Fever - drug therapy
Glycosides - pharmacology
Glycosides - therapeutic use
indica
Mangifera
Mangifera - chemistry
Mangifera indica
Mangiferin
Mice
Phytotherapy
Plant Bark - chemistry
Plant Extracts - pharmacology
Plant Extracts - therapeutic use
Saccharomyces cerevisiae
Treatment Outcome
Xanthones - administration & dosage
Xanthones - chemical synthesis
Xanthones - pharmacology
Xanthones - therapeutic use
title Synthesis and evaluation of novel analogues of mangiferin as potent antipyretic
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